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Synthesis and Anti‐HBV Activities Evaluation of New Ethyl 8‐Imidazolylmethyl‐7‐hydroxyquinoline‐3‐carboxylate Derivatives in vitro
Author(s) -
Liu Yajing,
Zhao Yanfang,
Zhai Xin,
Liu Xiuping,
Sun Lixue,
Ren Yanxia,
Gong Ping
Publication year - 2008
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200800035
Subject(s) - hbeag , hbsag , chemistry , carboxylate , in vitro , lamivudine , hepatitis b virus , 8 hydroxyquinoline , transfection , virology , virus , stereochemistry , biochemistry , biology , organic chemistry , gene
Some new ethyl 8‐imidazolylmethyl‐7‐hydroxyquinoline‐3‐carboxylate derivatives have been synthesized and evaluated for their anti‐hepatitis B virus (HBV) activities and cytotoxicities in HepG2.2.15 cells stable transfection with HBV. Compounds 13a , 11b , 11c , 12c , 13c , 11g , and 12g inhibited the expression of the viral antigens HBsAg or HBeAg in a low concentration, of which 11c (IC 50 = 12.6 μM, SI = 12.4), 12c (IC 50 = 3.5 μM, SI = 37.9), and 12g (IC 50 = 2.6 μM, SI = 61.6) showed more active abilities to inhibit the replication of HBV DNA than the positive control lamivudine ( 3TC , IC 50 = 343.2 μM, SI = 7.0).